Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/31—Hydrocarbons
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
  • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

• This invention relates to the discovery that candelilla wax and a certain fraction thereof affords an effective topical treatment for certain inflammatory skin conditions.
• Candelilla wax is the wax obtained from the Candelilla plant and consists largely of hydrocarbons. It has now been found that candelilla wax and a certain fraction of the wax possess substantial vasoconstrictive activity suitable for topically treating inflammation in humans or animals. Said fraction consists essentially of a mixture of saturated straight chain C 29-33 hydrocarbons, as represented by the formula: CH 3 --(CH 2 ) n --CH 3 , wherein n is an integer from 27 to 31, with the predominant hydrocarbon, about 80-85 percent by weight of the mixture, having a total of 31 carbons.
• Treating acne is used to mean the temporary alleviation of the inflammation of the affected skin and other inflammatory signs and symptoms associated with acne.
• the superior vasoconstrictor activity of candelilla wax itself and the subject hydrocarbon fraction afford the usage thereof in an effective anti-inflammatory treatment for the following skin disorders: atopic dermatitis, atopic eczema, herpes simplex, shingles, poison ivy, poison oak, poison sumac and other skin allergic reactions, psoriasis, dandruff, and the like.
• anti-inflammatory treatment or its equivalent is used to mean the temporary alleviation of the inflammation of the affected skin and other inflammatory signs and symptoms associated with the particular skin disorder.
• Suitable pharmaceutical carriers for the topical administration of candelilla wax and the subject hydrocarbon fraction are non-polar pharmaceutical vehicles in conventional forms such as solutions, lotions, emulsions, ointments, gels, etc., in which the pharmaceutical carrier merely provides a physical form for the effective topical application of the active component to the skin.
• the therapeutic composition is prepared by simply mixing the desired therapeutically effective amount of the candelilla wax or the hydrocarbon fraction with the particular carrier according to conventional pharmaceutical compounding techniques.
• a “therapeutically effective amount” is meant an amount which is effective to alleviate the inflammation of the dermatological condition and yet cause substantially no undesirable side effects (at a reasonable benefit/risk ratio).
• the candelilla wax and the subject hydrocarbon fraction are each therapeutically effective from about 0.1 to about 10 percent by weight, based on the composition weight, with from about 0.5 to about 5 percent by weight being preferred, and from about 2 to about 5 percent by weight being most preferred.
• a glass column 50 cm in length and 3 cm in diameter is dry-packed with Silica Gel 60 of particle size 0.063-0.200 mm (70-230 mesh ASTM); purchased from E. Merck Chemical Co.
• the Silica Gel is oven-dried at 120° C. for 4 to 6 hours prior to use.
• 50 Grams of candelilla wax is dissolved in 500 mls of warm hexane and the mixture is passed through the column at ambient temperature.
• the eluent is collected in a suitable glass vessel.
• the column is then eluted with an additional 1000 mls of hexane.
• non-polar organic solvents may be used to extract the hydrocarbon fraction from candelilla wax such as, for example, an aliphatic alkane such as pentane, heptane and the like; an aromatic hydrocarbon such as benzene, toluene, xylene and the like; an ether such as diethyl ether, dioxane and the like; tetrahydrofuran; and the like aprotic solvents.
• aprotic solvents as eluents, it is preferred to use a polar stationary phase such as, for example, silica gel, in the chromatographic separation step.
• the subject hydrocarbon fraction may be derived from candelilla wax by:
• TLC Thin Layer Chromotography
• the instant invention thus provides a pharmaceutical composition for alleviating inflammation associated with skin disorders comprising a therapeutically effective anti-inflammatory amount of candelilla wax or a substantially non-polar hydrocarbon fraction derived from candelilla wax and a pharmaceutical carrier suitable for topical administration, said candelilla wax fraction consisting essentially of a mixture of saturated straight chain hydrocarbons, wherein the chain length of said hydrocarbons is from C 29 to C 33 and about 80-85 percent by weight of said mixture is the C 31 hydrocarbon.
• the amount of each hydrocarbon in the aforementioned hydrocarbon mixture may range from about to about the following indicated percentages by weight:
• the C 31 hydrocarbon itself provides, as the predominant component of the mixture, and as exemplified hereinafter, a substantial part of the vasoconstrictive activity attributable to the subject hydrocarbon mixture, and, as such, can be used alone, thereby providing another aspect of this invention.
• the C 31 hydrocarbon itself may be utilized in the same manner and in the same amounts as herein described for candelilla wax itself or the hydrocarbon fraction derived therefrom, although from about 1 to about 10 percent by weight of the C 31 hydrocarbon is preferred when used by itself in the method and composition of this invention.
• a particularly suitable pharmaceutical carrier in ointment form for purposes of this invention is Hydrophilic Ointment U.S.P., an oil-in-water emulsion ointment base having the formulation:
• the stearyl alcohol and the white petrolatum are melted on a steam bath and warmed to about 75° C.
• the other ingredients are dissolved in the purified water and also heated to 75° C.
• the petrolatum phase is then added to the water phase with mixing until the mixture congeals.
• the resultant ointment is cooled to room temperature.
• vasoconstriction activity of candelilla wax, the subject hydrocarbon fraction and the C 31 hydrocarbon itself is demonstrated in the following invivo vasoconstrictor assay, which is a modification of the McKenzie-Stoughton Vasoconstrictor Assay described in "Method for Comparing Percutaneous Absorption of Steroids", Arch. Derm. 86:608-610, 1962.
• test formulations were applied under semi-occlusion to maximize differences in activity.
• test formulations are saturated on the absorbent cushion pad of 3/4 inch bandages (Curity Curad Sheer Bandages) and the bandages taped to the forearm with no more than 7 bandages per forearm.
• the bandages are left on the forearm for 24 hours and then removed.
• the treatment sites are washed with soap and water to remove any excess material still on the skin surface. After 1 hour, the resulting blanching or whitening of the skin is then scored by two judges using the following scoring system:
• An increase in blanching reflects a corresponding increase in vasoconstriction activity.
• LIDEX Cream 0.05% induced a very high vasoconstrictive effect with a maximum score of 3.0.
• Both candelilla wax preparations were substantially comparable to LIDEX Cream 0.05%.
• the C 31 hydrocarbon itself had a demonstrable score of 1.5 even at the low 1% concentration.
• the hydrophilic ointment vehicle induced a slight blanching effect with a score of 1.0.
• both candelilla wax and the subject hydrocarbon fraction are each deemed to be of value as a therapeutic agent for treatment of inflammatory skin disorders.
• the amount of composition typically applied and treatment regimen will vary, depending upon, for example, the particular disorder being treated and its severity, the frequency of application and the area of the body which is afflicted.
• the preferred treatment will comprise applying a therapeutically effective amount of the composition to the afflicted situs on the skin.
• a therapeutically effective amount would be from about 1 mg/cm 2 to about 10 mg/cm 2 , and preferably about 2-5 mg/cm 2 , of the composition per day. It is preferred to cleanse the skin prior to treatment. The treatment is more effective if topical applications are made 2 to 4 times daily.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Dermatology (AREA)
• Rheumatology (AREA)
• Pain & Pain Management (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicines Containing Plant Substances (AREA)
• Cosmetics (AREA)

Priority Applications (8)

Applications Claiming Priority (1)

Publications (1)

Family

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Family Applications (1)

Country Status (8)

Cited By (6)

Citations (4)

Family Cites Families (1)

• 1984
  • 1984-10-15 US US06/660,899 patent/US4758432A/en not_active Expired - Fee Related
• 1985
  • 1985-09-19 AU AU47593/85A patent/AU584120B2/en not_active Ceased
  • 1985-09-20 ZA ZA857257A patent/ZA857257B/xx unknown
  • 1985-09-23 NZ NZ213580A patent/NZ213580A/en unknown
  • 1985-09-26 CA CA000491602A patent/CA1266618A/en not_active Expired - Lifetime
  • 1985-10-14 JP JP60227054A patent/JPS61251626A/ja active Pending
  • 1985-10-14 DK DK468885A patent/DK468885A/da not_active Application Discontinuation
  • 1985-10-14 EP EP85113026A patent/EP0178623A3/en not_active Ceased

Patent Citations (5)

Non-Patent Citations (1)

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